SJF-1528

SJF-1528 (PROTAC 1) is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutant EGFR in HeLa cells. SJF-1528 also degrades HER2. SJF-1528 promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (Pink: ligand for target protein (HY-159047) ; Black: linker Tos-PEG2-CH2-Boc (HY-130532) ; Blue: ligand for E3 ligase (S, R, S) -AHPC (HY-125845) ) [1].

Product Specifications

CAS Number

[2230821-38-0]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

EGFR; PROTACs

Type

Reference compound

Related Pathways

JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sjf-1528.html

Purity

99.71

Solubility

DMSO : 103.06 mg/mL (ultrasonic; warming)

Smiles

O=C([C@H]1N(C([C@@H](NC(COCCOCCOC2=CC=C(C3=CC4=C(NC5=CC=C(OCC6=CC=CC(F)=C6)C(Cl)=C5)N=CN=C4C=C3)C=C2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7

Molecular Formula

C55H57ClFN7O8S

Molecular Weight

1030.60

Precautions

H315, H319, H320

References & Citations

[1]Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25 (1) :67-77.e3.